AMG 511|cas:1253573-53-3|西域试剂

AMG 511,99.38%

产品编号：Bellancom-13440| CAS NO：1253573-53-3| 分子式：C₂₂H₂₈FN₉O₃S| 分子量：517.58

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货号	价格	库存与货期
Bellancom-13440	￥2200.00	杭州北京（现货）
Bellancom-13440	￥4200.00	杭州北京（现货）
Bellancom-13440	￥9400.00	杭州北京（现货）

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AMG 511

产品介绍

AMG 511 是一个高效、口服有效的 I 类 pan-PI3K 抑制剂,对 PI3Kα, β, δ 和 γ 作用的 K_i 值分别为 4 nM, 6 nM, 2 nM 和 1 nM。AMG 511 减少 p-Akt (Ser473), 体现了它显著抑制了 PI3K 信号。AMG 511 在小鼠胶质母细胞瘤移植瘤模型中具有抗肿瘤活性。

生物活性

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with K_is of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.

体外研究

AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC₅₀ of 4 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days).
AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:	Oral administration, daily, for 12 days
Result:	Inhibited tumor growth.

Animal Model:	Male Sprague-Dawley rats
Dosage:	1 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:	Oral administration, daily, for 12 days
Result:	Inhibited tumor growth.

Animal Model:	Male Sprague-Dawley rats
Dosage:	1 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9321 mL	9.6603 mL	19.3207 mL
5 mM	0.3864 mL	1.9321 mL	3.8641 mL
10 mM	0.1932 mL	0.9660 mL	1.9321 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (3.86 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (3.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明